The objective of this project is the discovery of new types of clinically useful anticancer drugs. The following topics are of current interest: (1) nucleosides, reduced nucleosides and the chemistry of 5-azacytidine, (2) target specific agents for CNS and lung tumors, (3) pyridones and phenalkylamines as antitumor agents and (4) transition-state enzyme inhibitors. BIBLIOGRAPHIC REFERENCES: Driscoll, J.S. and Beisler, J.A.: Antineoplastic Agents. In Clarke, F.H. (Ed.): Annual Reports in Medicinal Chemistry, Vol. 12, Academic Press, N.Y., 1977, in press. Voytek, P., Beisler, J.A., Abbasi, M.M. and Wolpert-DeFillipes, M.K.: Comparative Studies of the Cytostatic Action and Metabolism of 5-Azacytidine and 5,6-Dihydro-5-azacytidine. Cancer Res., 37: 1956-1961, 1977.